2-[2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)ethyl]-5H-imidazo[2,1-a]isoindole | 1376768-90-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并吡嗪类
• 英文名称: 2-[2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)ethyl]-5H-imidazo[2,1-a]isoindole
• 英文别名: US8796304, 2-[2-(5,8-Bis(trideuteromethyl)-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)-ethyl]-5,5-dideutero-5H-imidazo[2,1-a]isoindole
• CAS: 1376768-90-9
• 化学式: C₁₉H₁₈N₆
• 分子量: 330.392
• InChiKey: DBMVTWOKPCPULJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  60.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-[2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)ethyl]-5H-imidazo[2,1-a]isoindole 在 双氧水 作用下， 以 水 、 溶剂黄146 为溶剂， 反应 12.0h， 以20%的产率得到2-[-2-(5,8-Dimethyl-7-oxy-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)-ethyl]-5H-imidazo[2,1-a]isoindole
  参考文献：
  名称：

  Imidazole derivatives as PDE10A enzyme inhibitors

  摘要：

  这项发明涉及一类PDE10A酶抑制剂化合物。该发明提供了一种包含该发明化合物的治疗有效量和药用载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了一种治疗神经退行性疾病的方法，包括向患有神经退行性疾病的受试者施用式I化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患有药物成瘾的受试者施用式I化合物的治疗有效量。本发明还提供了一种治疗精神障碍的方法，包括向患有精神障碍的受试者施用式I化合物的治疗有效量。

  公开号：

  US20120129836A1
• 作为产物：
  描述：

  2-<(2-Cyan-phenyl)methyl>-2H-isoindol-1,3-dion 在 palladium 10% on activated carbon 氢气 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 、 potassium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 、 乙腈 为溶剂， 反应 34.5h， 生成 2-[2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)ethyl]-5H-imidazo[2,1-a]isoindole
  参考文献：
  名称：

  Imidazole derivatives as PDE10A enzyme inhibitors

  摘要：

  这项发明涉及一类PDE10A酶抑制剂化合物。该发明提供了一种包含该发明化合物的治疗有效量和药用载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了一种治疗神经退行性疾病的方法，包括向患有神经退行性疾病的受试者施用式I化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患有药物成瘾的受试者施用式I化合物的治疗有效量。本发明还提供了一种治疗精神障碍的方法，包括向患有精神障碍的受试者施用式I化合物的治疗有效量。

  公开号：

  US20120129836A1

文献信息

• [EN] IMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS<br/>[FR] DÉRIVÉS D'IMIDAZOLE UTILISÉS COMME INHIBITEURS D'ENZYMES PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2013107856A1

  公开（公告）日：2013-07-25

  This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

  这项发明涉及一种PDE10A酶抑制剂化合物。该发明提供了包括该发明化合物的治疗有效量和药用载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了一种治疗患有神经退行性疾病的受试者的方法，包括向受试者投予式I化合物的治疗有效量。本发明还提供了一种治疗患有药物成瘾的受试者的方法，包括向受试者投予式I化合物的治疗有效量。本发明还提供了一种治疗患有精神障碍的受试者的方法，包括向受试者投予式I化合物的治疗有效量。
• Tricyclic imidazole compounds as PDE10 inhibitors
  申请人：Kehler Jan

  公开号：US08552045B2

  公开（公告）日：2013-10-08

  This invention is directed to compounds with the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula 1. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula 1. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula 1. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula 1.

  本发明涉及具有下列结构的化合物，其为PDE10A酶抑制剂。本发明提供了一种制药组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明还提供了制备式1化合物的方法。本发明进一步提供了一种治疗神经退行性疾病的方法，包括向患者施用式1化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患者施用式1化合物的治疗有效量。本发明进一步提供了一种治疗精神障碍的方法，包括向患者施用式1化合物的治疗有效量。
• Substituted imidazo[2,1-A]isoindoles as PDE10 inhibitors
  申请人：H. Lundbeck A/S

  公开号：US09062060B2

  公开（公告）日：2015-06-23

  This invention is directed to compounds with the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

  本发明涉及结构为的化合物，其为PDE10A酶抑制剂。本发明提供了一种制药组合物，包括本发明中化合物的治疗有效量和药学上可接受的载体。本发明还提供了制备公式I化合物的方法。本发明还提供了一种治疗神经退行性疾病患者的方法，包括向患者施用公式I化合物的治疗有效量。本发明还提供了一种治疗药物成瘾患者的方法，包括向患者施用公式I化合物的治疗有效量。本发明还提供了一种治疗精神障碍患者的方法，包括向患者施用公式I化合物的治疗有效量。
• Imidazole derivatives as PDE10 enzyme inhibitors
  申请人：H. Lundbeck A/S

  公开号：US20140357639A1

  公开（公告）日：2014-12-04

  This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

  本发明涉及一种PDE10A酶抑制剂化合物。该发明提供了一种药物组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明还提供了制备公式I化合物的方法。本发明还提供了一种治疗神经退行性疾病的方法，包括向患者施用公式I化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患者施用公式I化合物的治疗有效量。本发明还提供了一种治疗精神疾病的方法，包括向患者施用公式I化合物的治疗有效量。
• IMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS
  申请人：H. Lundbeck A/S

  公开号：EP2640731A1

  公开（公告）日：2013-09-25